P118
ファクロフェン
solid
別名:
3-アミノ-2-(4-クロロフェニル)プロパンホスホン酸
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この商品について
実験式（ヒル表記法）:
C9H13ClNO3P
CAS番号:
分子量:
249.63
NACRES:
NA.32
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
製品名
ファクロフェン, solid
InChI key
VSGNGLJPOGUDON-UHFFFAOYSA-N
SMILES string
NCC(CP(O)(O)=O)c1ccc(Cl)cc1
InChI
1S/C9H13ClNO3P/c10-9-3-1-7(2-4-9)8(5-11)6-15(12,13)14/h1-4,8H,5-6,11H2,(H2,12,13,14)
form
solid
impurities
≥97% (NMR)
color
white
solubility
0.1 M HCl: 13.3 mg/mL
methanol: 19.3 mg/mL
DMSO: insoluble
Quality Level
Gene Information
human ... GABBR1(2550), GABBR2(9568)
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Application
Phaclofen has been used to block GABAB receptor.
Biochem/physiol Actions
Phaclofen plays a vital role in identifying the physiological importance of central and peripheral bicuculline-insensitive receptors with which GABA and (−) baclofen interact. Phaclofen acts as a GABAB receptor antagonist. Phaclofen has an ability to reversibly block the late, bicuculline resistant, K+ dependent inhibitory postsynaptic potential (IPSP) logged in projection cells of the cat and rat dorsal lateral geniculate nucleus and in rat hippocampal CA1 pyramidal neurons.
General description
Phaclofen is a phosphonic acid derivative of baclofen.
signalword
Warning
hcodes
Hazard Classifications
Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
target_organs
Respiratory system
保管分類
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
dust mask type N95 (US), Eyeshields, Gloves
The GABAB antagonist phaclofen inhibits the late K+-dependent IPSP in cat and rat thalamic and hippocampal neurones
Soltesz I, et al.
Brain Research, 448(2), 351-354 (1988)
Effat Ramshini et al.
International journal of preventive medicine, 4(2), 158-164 (2013-04-02)
There is only little information about the effects of GABA receptors agonist and antagonist on morphine self-administration. Present study was designed to assess role of GABAB receptors in the regulation of morphine-reinforced self-administration. THIS STUDY WAS PERFORMED IN FOUR GROUPS
Kazuo Kunisawa et al.
European journal of pharmacology, 796, 122-130 (2016-12-13)
GABA mediated neuronal system regulates hippocampus-dependent memory and stress responses by controlling plasticity and neuronal excitability. Here, we demonstrate that betaine ameliorates water-immersion restraint stress (WIRS)-induced memory impairments. This improvement was inhibited by a betaine/GABA transporter-1 (GABA transporter-2: GAT2) inhibitor
Luminal administration ex vivo of a live Lactobacillus species moderates mouse jejunal motility within minutes.
Wang B, et al.
Faseb Journal, 24(10), 4078-4088 (2010)
H Hasuo et al.
Neuroscience letters, 86(1), 77-81 (1988-03-21)
Phaclofen has recently been described as an antagonist to baclofen at both peripheral and central receptors. We have applied phaclofen in known concentrations to an isolated rat brain slice preparation containing the septal nuclei. Our data demonstrate that phaclofen antagonizes
ライフサイエンス、有機合成、材料科学、クロマトグラフィー、分析など、あらゆる分野の研究に経験のあるメンバーがおります。.
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